modafinil PROVIGIL
Class: Wakefulness-promoting AgentFDA Indications: Narcolepsy, Shift Work Sleep Disorder (SWSD), Obstructive Sleep Apnea/Hypopnea Syndrome (OSAHS), Narcolepsy
Off-Label Use: Jet Lag, Treatment Resistant Depression, ADHD, Cocaine Addiction, Sleepiness Associated With Opioid Analgesia, Lewy Body Dementia
Prescribing
FDA Schedule IVForms: 100, 200mg tablet
Dose Range: 200-800 mg/day
Starting: 200 mg qam is usual dose; max dose 800 mg daily
Stopping: Tapering unnecessary, though some patients may have sleepiness on discontinuation
Precautions
Contraindications: Not recommended for use in patients with a h/o LVH, ischemic ECG Δ's, chest pain, arrhythmias or recent MISerious Side Effects: Stevens-Johnson Syndrome
Side Effects: headache (34%), anxiety, insomnia, xerostomia, diarrhea, nausea, rhinitis/rhinorrhea, palpitations, hypertension
Pharmacodynamics
1° MOA: Exact mechanism of action is unknown, but it is believed that the increase in synaptic dopamine following blockade of DAT leads to increased tonic firing and downstream effects on neurotransmitters including those involved in wakefulness, such as histamine and orexin/ hypocretinTarget: DAT, D2 partial agonist
Pharmacokinetics
t½: 15° TMAX: 2-4°Substrate of: 3A4
Inhibits: 2C19; Induces: 3A4
Active Metabolites: ∅
DDIs
- - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers (including itself) can ↓ levels
- - as a 2C9/2C19 inhibitor, can ↑ levels of co-prescribed 2C9/2C19 substrates as a 3A4 inducer, can ↓ levels of co-prescribed 3A4 substrates
Misc
- - has as novel mechanism of action and therapeutic uses with less abuse potential, but is often classified as a stimulant
- - binds at the DAT and is only about eightfold less potent than cocaine as a DAT inhibitor
- - α1 antagonists (e.g., prazosin) may block its therapeutic actions
- - may be useful in treating fatigue in patients with depression, multiple sclerosis, myotonic dystrophy and HIV/AIDS
- - subjective sensation is generally normal wakefulness, not stimulation, but can occasionally include jitteriness
- - may induce its own metabolism at high doses via 3A4 induction
Special Populations
Category Undefined.—Animal data suggest moderate risk, but limited human pregnancy experience prevents a full assessment of risk. Avoiding modafinil during pregnancy is the best course, but inadvertent exposure does not appear to represent a major risk of embryo-fetal harm
No reports describing the use of modafinil during human lactation have been located
Clearance of modafinil may be reduced in the elderly
There is inadequate information to determine safety and efficacy of dosing in patients with severe renal impairment
Dose should be reduced in patients with severe hepatic impairment
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